Synthesis of 4-pyrido-6-aryl-2-substituted amino pyrimidines as a new class of antimalarial agents

Anu Agarwal; Kumkum Srivastava; S K Puri; Prem M S Chauhan

doi:10.1016/j.bmc.2005.06.052

Synthesis of 4-pyrido-6-aryl-2-substituted amino pyrimidines as a new class of antimalarial agents

Bioorg Med Chem. 2005 Nov 15;13(22):6226-32. doi: 10.1016/j.bmc.2005.06.052. Epub 2005 Jul 28.

Authors

Anu Agarwal¹, Kumkum Srivastava, S K Puri, Prem M S Chauhan

Affiliation

¹ Division of Medicinal AND Process Chemistry, Central Drug Research Institute, Lucknow 226001, India.

PMID: 16054819
DOI: 10.1016/j.bmc.2005.06.052

Abstract

A series of 2,4,6-trisubstituted pyrimidines were synthesized and evaluated for their in vitro antimalarial activity against Plasmodium falciparum. Of the 18 compounds synthesized, 14 compounds showed MIC in the range of 0.25-2 microg/mL. These compounds are in vitro several fold more active than pyrimethamine.

Publication types

Comparative Study
Research Support, Non-U.S. Gov't

MeSH terms

Animals
Antimalarials / chemical synthesis*
Antimalarials / chemistry
Antimalarials / therapeutic use
Diamines / chemistry
Models, Chemical
Parasitic Sensitivity Tests
Plasmodium falciparum / drug effects*
Pyridines / chemistry
Pyrimethamine / therapeutic use
Pyrimidines / chemical synthesis*
Pyrimidines / chemistry
Pyrimidines / therapeutic use*

Substances

Antimalarials
Diamines
Pyridines
Pyrimidines
pyridine
Pyrimethamine